US 5,962,455 AGranted

Certain substituted benzylamine derivatives a new class of neuropeptide Y1 specific ligands

AssigneeNeurogen Corporation

InventorsCharles A. Blum, Alan Hutchison, John M. Peterson

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Abstract

This invention encompasses compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein X.sub.1, X.sub.2, X.sub.3 represent organic or inorganic substituents, n is 1, 2, or 3, m is 2, 3, or 4, R.sub.1 -R.sub.4 are hydrogen or organic substituents, and B is nitrogen, carbon, sulfur or oxygen, useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to mammalian Neuropeptide Y1 receptors.

Claims11

Dependent claims

A compound of the formula:

##STR17## wherein one of X.sub.1, X.sub.2 and X.sub.3 is ##STR18## and the remaining members of the group of X.sub.1, X.sub.2 and X.sub.3 are hydrogen;
where Y is an aryl group selected from the group consisting of phenyl, 2-,3-, or 4-pyridyl, naphthyl, 2-, 3-, 4-, or 6-quinolyl, 3- or 4-isoquinolyl, 2- or 6-quinoxalyl, and 3-(1,8-naphthyridyl), each of which is optionally mono- or disubstituted with halogen, hydroxy, straight or branched chain C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy;
R.sub.o and R.sub.p are the same or different and represent hydrogen-, straight or branched chain alkyl having 1-6 carbon atoms, arylalkyl wherein the alkyl portion is straight or branched chain lower alkyl having 1-6 carbon atoms or R.sub.o and R.sub.p together may represent --(CH.sub.2).sub.n-- where n is 1, 2 or 3;
and
Ar is phenyl which is optionally mono- or disubstituted with halogen, hydroxy, or straight or branched chain lower alkyl having 1-6 carbon atoms;
m is 2,
R.sub.1 and R.sub.2 are the same or different and represent hydrogen, or straight or branched chain lower alkyl having 1-6 carbon atoms;
R.sub.3 and R.sub.4 are the same or different and represent hydrogen, straight or branched chain lower alkyl having 1-6 carbon atoms, or straight or branched chain lower alkoxy having 1-6 carbon atoms;
R.sub.5 represents straight or branched chain lower alkyl having 1-6 carbon atoms, phenyl, 2-, 3-, or 4-pyridyl, or phenyl, 2-, 3-, or 4-pyridyl straight or branched chain lower alkyl having 1-6 carbon atoms;
and
R.sub.6 represents hydrogen, hydroxyl, amino, straight or branched chain lower alkyl having 1-6 carbon atoms, straight or branched chain lower alkoxy having 1-6 carbon atoms, phenyl, 2-, 3-, or 4-pyridyl, phenoxy, 2-, 3-, or 4-pyridyloxy, or
--(CH.sub.2).sub.r --A'--(CH.sub.2).sub.q --B'
where
r is 0-5, q is 1-5, and A' is a direct bond, oxygen or sulfur, and
B' is hydrogen, straight or branched chain lower alkyl having 1-6 carbon atoms, straight or branched chain lower alkoxy having 1-6 carbon atoms, phenyl, 2-, 3-, or 4-pyridyl, phenoxy, 2-, 3-, or 4-pyridyloxy, carboxyl, carboalkoxy, carboxamido, mono or dialkylcarboxamido, amino, or mono or dialkylamino;
and pharmaceutically acceptable salts thereof.

13 more elements

Dependencies are inferred from the claim text.

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Abstract

A compound of the formula:

##STR17## wherein one of X.sub.1, X.sub.2 and X.sub.3 is ##STR18## and the remaining members of the group of X.sub.1, X.sub.2 and X.sub.3 are hydrogen;
where Y is an aryl group selected from the group consisting of phenyl, 2-,3-, or 4-pyridyl, naphthyl, 2-, 3-, 4-, or 6-quinolyl, 3- or 4-isoquinolyl, 2- or 6-quinoxalyl, and 3-(1,8-naphthyridyl), each of which is optionally mono- or disubstituted with halogen, hydroxy, straight or branched chain C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy;
R.sub.o and R.sub.p are the same or different and represent hydrogen-, straight or branched chain alkyl having 1-6 carbon atoms, arylalkyl wherein the alkyl portion is straight or branched chain lower alkyl having 1-6 carbon atoms or R.sub.o and R.sub.p together may represent --(CH.sub.2).sub.n-- where n is 1, 2 or 3;
and
Ar is phenyl which is optionally mono- or disubstituted with halogen, hydroxy, or straight or branched chain lower alkyl having 1-6 carbon atoms;
m is 2,
R.sub.1 and R.sub.2 are the same or different and represent hydrogen, or straight or branched chain lower alkyl having 1-6 carbon atoms;
R.sub.3 and R.sub.4 are the same or different and represent hydrogen, straight or branched chain lower alkyl having 1-6 carbon atoms, or straight or branched chain lower alkoxy having 1-6 carbon atoms;
R.sub.5 represents straight or branched chain lower alkyl having 1-6 carbon atoms, phenyl, 2-, 3-, or 4-pyridyl, or phenyl, 2-, 3-, or 4-pyridyl straight or branched chain lower alkyl having 1-6 carbon atoms;
and
R.sub.6 represents hydrogen, hydroxyl, amino, straight or branched chain lower alkyl having 1-6 carbon atoms, straight or branched chain lower alkoxy having 1-6 carbon atoms, phenyl, 2-, 3-, or 4-pyridyl, phenoxy, 2-, 3-, or 4-pyridyloxy, or
--(CH.sub.2).sub.r --A'--(CH.sub.2).sub.q --B'
where
r is 0-5, q is 1-5, and A' is a direct bond, oxygen or sulfur, and
B' is hydrogen, straight or branched chain lower alkyl having 1-6 carbon atoms, straight or branched chain lower alkoxy having 1-6 carbon atoms, phenyl, 2-, 3-, or 4-pyridyl, phenoxy, 2-, 3-, or 4-pyridyloxy, carboxyl, carboalkoxy, carboxamido, mono or dialkylcarboxamido, amino, or mono or dialkylamino;
and pharmaceutically acceptable salts thereof.

13 more elements